Nanoemulsion Formulation Services

As a leading biopharmaceutical company, BOC Sciences is focused on providing cutting-edge nanoemulsion formulation services that provide innovative solutions to enhance drug delivery. Nanoemulsions have great potential to improve the bioavailability and stability of drug compounds due to their unique properties.

What is the difference between emulsion and nanoemulsion?

Nanoemulsions are sub-micron sized emulsions, typically between 20 and 200 nanometers, with unique properties that make them ideal for drug delivery systems. Unlike conventional emulsions, nanoemulsions offer better hydrophobic drug solubility, greater stability, controlled release properties, and enhanced bioavailability. These fine dispersions, consisting of oil, water, surfactants, and sometimes cosurfactants, allow for more efficient delivery of active pharmaceutical ingredients (APIs) through biological systems.

What are nanoemulsion formulation techniques?

Depending on the underlying physicochemical mechanism of droplet rupture, there are two main methods for the formation of nanoemulsions: high energy external emulsification (high pressure homogenization, microjet, ultrasonic, etc.) and low energy emulsification (e.g. emulsion phase conversion (EPI), spontaneous emulsification).

Fig. 1 General formulation approach of nanoemulsions using high-energy methods. (Gawin-Mikołajewicz, A., 2021)

High pressure homogenization

High pressure homogenization is that under high pressure, the material is subjected to strong shear force and pressure to achieve crushing and emulsifying effect. The main causes of shear force and compression are hole effect, laminar effect and ray-current effect. The high pressure homogenizer can provide the energy required by the system in a short time, and obtain the conventional properties of nanoemulsion.

Ultrasonic emulsification

Ultrasonic emulsification method is a method that uses ultrasonic device to make the non-phase solution in the system to crush and disperse evenly, and form emulsion with the surrounding liquid. Compared with the conventional emulsification method, ultrasonic emulsification has the advantages of small particle size, stable emulsification system and low power requirement. Although phacoemulsification has a significant effect in reducing particle size, it can only be used in laboratory research or small batch production, so its application is limited.

Microjet emulsification

The microjet emulsification method uses the microjet high pressure homogenization equipment and the high pressure pump to make the material enter the reaction chamber. In the reaction chamber, the raw material is divided into multiple streams to form high-speed fluids, and enters the impact zone of the reaction chamber in a high-speed jet state for ultra-high frequency shear, while the jet passes through a more intense vertical collision. Most of the energy is released during the collision, resulting in 90 percent of the pressure drop. In the impact zone, there is shearing and mutual impact between the materials, which makes the liquid drops in the material highly broken and realizes the homogeneous emulsification of the material.

Phase inversion temperature method

The phase inversion temperature method is based on the fact that the molecular geometry of nonionic surfactants changes with the change of temperature. In the ternary system containing water-oil-surfactant, when the temperature of the system is raised to the phase transition temperature, the spontaneous curvature of the surfactant is close to 0, and the surface tension is the lowest at this time, and then the system is cooled instantaneously, that is, the nanoemulsion with small particle size is obtained. At low temperature, the spontaneous curvature of the surfactant is large positive, which is conducive to the formation of stable oil-in-water (O/W). Lotion. At high temperatures, the spontaneous curvature of the surfactant is a large negative value, which is conducive to the formation of a stable water-in-oil (W/O) emulsion.

Phase inversion composition (PIC)

Phase inversion composition method is a method of gradually adding water to a certain proportion of oil-surfactant solution at a constant temperature. With the increase of water content, the surfactant undergoes the opposite revolution, and finally the O/W nanoemulsion is obtained, so this method is called the reverse transformation method.

Self-emulsification

Self-emulsification method, namely microemulsion dilution method, forms nano-particles by using chemical energy released in the process of microemulsion dilution. During the dilution process, the system has no phase change, that is, the spontaneous curvature of surfactant has no positive or negative change, which is an important difference between microemulsion dilution method and inverse emulsification and phase transition temperature method.

Advantages of nanoemulsion drug delivery system

Nanoemulsions have several advantages as drug delivery systems, making them the first choice for enhancing drug efficacy.

Improve bioavailability: Nanoemulsions can improve the solubility and absorption of drugs with poor water solubility, thereby increasing their bioavailability. The small droplet size and large surface area are conducive to the rapid dissolution and absorption of drugs.

Targeted drug delivery: Nanoemulsions can be designed to target specific tissues or cells, thereby reducing off-target effects and improving therapeutic outcomes. Surface modification using ligands or antibodies enables targeted delivery to the diseased site.

Controlled release: The nanoemulsion can control and continuously release the drug, ensuring a long-term stable therapeutic effect. This reduces the frequency of dosing and improves patient compliance.

Improve stability: Nanoemulsions can improve the stability of encapsulated drugs, prevent drug degradation and extend their shelf life. The surfactants and stabilizers used in the nanoemulsion formulation prevent drug precipitation and aggregation.

Versatility: Nanoemulsions can be used in a variety of drugs, including hydrophilic, lipophilic and amphiphilic compounds. They are suitable for a variety of routes of administration, such as oral, topical, intravenous and pulmonary.

Our expertise in nanoemulsion formulations

Nanoemulsion formulation design and optimization

Design and optimize the formulation of nanoemulsion according to the specific needs of customers, such as drug type, target disease, drug delivery route, etc. This includes selecting the appropriate oil phase, water phase, and emulsifier, as well as determining the optimal preparation conditions (such as temperature, pressure, stirring speed, etc.) to ensure emulsion stability, biocompatibility, and drug loading efficiency.

Nanoemulsion preparation technology development

The use of advanced preparation technology, such as high pressure homogenization, ultrasonic dispersion, microfluidic technology, etc., to accurately control the size distribution, morphology and surface properties of nanoemulsion to improve its physicochemical stability and bioavailability.

Characterization of nanoemulsions

The conventional evaluation of nanoemulsions mainly includes emulsion type, droplet size and distribution, stability, appearance, pH value, viscosity, polydispersion index, drug encapsulation rate, zeta potential, compatibility and so on. Particle size was detected by laser particle size analyzer, and nanoemulsion morphology was detected by transmission electron microscopy (TEM).

In vitro and in vivo pharmacodynamic studies

Through cell experiments and animal models, the biological distribution, pharmacokinetic characteristics, targeting ability and therapeutic effect of nanoemulsion under different conditions were evaluated, as well as possible toxic and side effects, to provide scientific basis for subsequent clinical applications.

Stability testing and shelf life studies

Long-term and accelerated stability tests, tests at temperatures and humidity higher than conventional storage conditions and long-term monitoring under specified storage conditions, to observe the physical and chemical changes of the nanoemulsion under different storage conditions, determine the expiration date of the product, and ensure its safety and effectiveness during the expiration date.

Scale-up production and process optimization

Assisting customers to scale up lab-scale nanoemulsion preparation processes to pilot or industrial production levels, optimizing production processes, reducing costs, and increasing yields while maintaining consistent product quality.

Our experimental equipment capabilities

• High pressure homogenizer
• Ultrasonic processor
• Microfluidic chip system
• Transmission electron microscope (TEM)
• High performance liquid chromatography (HPLC)
• Flow cytometer

Our nanoemulsion service process

• Customer demand analysis
• Formulation design
• Preparation and optimization of nanoemulsion
• Evaluation and verification of nanoemulsion properties
• Large-scale production scheme
• Technical support and consultation

The unique properties of nanoemulsions, including their small droplet size, enhanced stability, and versatility, set them apart from traditional emulsions and open up new possibilities for drug delivery, transdermal applications, vaccines, cancer treatments, and even nutritional supplements. As a biopharmaceutical company committed to innovation, BOC Sciences offers a comprehensive range of nanoemulsion formulation services to provide customers with the most effective and advanced drug delivery solutions to facilitate the development and commercialization of innovative therapies.

FAQ

1. How can nanoemulsions benefit the pharmaceutical product?

Nanoemulsions enhance the solubility and bioavailability of poorly soluble drugs, improve drug stability, and enable controlled release. They can also facilitate targeted drug delivery and reduce side effects by allowing more precise delivery of therapeutic agents.

2. What types of drugs can be formulated into nanoemulsions?

Nanoemulsions can be used to formulate a wide range of drugs, including hydrophobic drugs, peptides, proteins, and nucleic acids. They are particularly beneficial for compounds with poor water solubility or stability issues.

3. What is the typical size range of the droplets in a nanoemulsion?

The droplet size in a nanoemulsion typically ranges from 20 to 200 nanometers. This small size range is crucial for maintaining the unique properties and stability of the nanoemulsion.

4. What methods do you use to prepare nanoemulsions?

We utilize various techniques to prepare nanoemulsions, including high-pressure homogenization, ultrasonic emulsification, and microfluidization. The method chosen depends on the specific characteristics and requirements of the formulation.

5. Can you customize nanoemulsions for specific applications?

Absolutely. We offer tailored formulation services to meet the specific needs of your application, whether it involves modifying the drug release profile, enhancing bioavailability, or targeting specific tissues or cells.

6. How do you ensure the stability of nanoemulsions?

We employ a variety of techniques to ensure the stability of our nanoemulsions, including the use of stabilizers and emulsifying agents, optimizing the pH and ionic strength of the formulation, and conducting extensive stability testing under different conditions.

7. What information do you need from us to start a nanoemulsion formulation project?

We require detailed information about the drug or active ingredient, including its solubility, stability, and intended route of administration. Additionally, specifics about the desired release profile and target application would be helpful.